Signal transducer and activator of transcription 3 (STAT3): a promising target for anticancer therapy

Future Med Chem. 2011 Apr;3(5):567-97. doi: 10.4155/fmc.11.22.


Signal transducer and activator of transcription 3 (STAT3) is an oncogenic protein whose inhibition is sought for the prevention and treatment of cancer. In this review, the validated therapeutic strategy to block aberrant activity of STAT3 in many tumor cell lines is evaluated by presenting the most promising inhibitors to date. The compounds are discussed in classes based on their different mechanisms of action, which are critically explained. In addition, their future clinical development as anticancer agents is considered. Furthermore, the efforts devoted to the comprehension of the structure-activity relationships and to the identification of the biological effects are brought to attention. The synthetic and technological approaches recently developed to overcome the difficulties in the obtainment of clinically suitable drugs are also presented.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Humans
  • Models, Molecular
  • Neoplasms / drug therapy*
  • STAT3 Transcription Factor / antagonists & inhibitors*
  • STAT3 Transcription Factor / chemistry
  • STAT3 Transcription Factor / metabolism*
  • Signal Transduction / drug effects


  • Antineoplastic Agents
  • STAT3 Transcription Factor